Kappa Opioid Receptor Expression and Function in Cells of the Immune System.

The kappa opioid receptor (KOR) is expressed on a number of hematopoietic cell populations, based on both protein binding analysis and the detection of kappa opioid receptor gene (Oprk1) transcripts. There are prominent Oprk1 splice variants that are expressed in the mouse and human brain cells and leukocytes. The activation of KOR results in reduced antibody production, an inhibition of phagocytic cell activity, an inhibition of T cell development, alterations in the production of various pro-inflammatory cytokines, chemokines, and the receptors for these mediators. Finally, the activation of KOR also leads to the regulation of receptor functional activity of chemokine receptors through the process of heterologous desensitization. The functional activity of KOR is important for the regulation of inflammatory responses and may provide opportunities for the development of therapeutics for the treatment of inflammatory disease states.